Pharmaceutical Sciences Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, 1417614411, Iran.
Faculty of Pharmacy, and Pharmaceutical Sciences Research Center, Shahid Sadoughi University of Medical Sciences, Yazd, Iran.
Eur J Med Chem. 2021 Feb 15;212:113034. doi: 10.1016/j.ejmech.2020.113034. Epub 2020 Nov 25.
The combination of heterocycles offers a new opportunity to create novel multicyclic compounds having improved biological activity. Coumarins are ubiquitous natural heterocycle widely adopted in the design of various biologically active compounds. Fusing different heterocycles with coumarin ring is one of the interesting approaches to generating novel hybrid molecules having highlighted biological activities. In the efforts to develop heterocyclic-fused coumarins, a wide range of 3,4-heterocycle-fused coumarins have been introduced bearing outstanding biological activity. The effect of heterocycles annulation at 3,4-positions of coumarin ring on the biological activity of the target structures were discussed. This review focuses on the important progress of 3,4-heterocycle-fused coumarins providing better insight for medicinal chemists on the design and preparation of biologically active heterocycle-fused coumarins with a significant therapeutic effect in the future.
杂环的组合为创造具有改善的生物活性的新型多环化合物提供了新的机会。香豆素是广泛存在的天然杂环，广泛应用于各种具有生物活性的化合物的设计中。将不同的杂环与香豆素环融合是生成具有突出生物活性的新型杂化分子的有趣方法之一。在开发杂环融合香豆素的努力中，已经引入了广泛的 3,4-杂环融合香豆素，具有出色的生物活性。讨论了香豆素环 3,4-位杂环环合对目标结构生物活性的影响。本综述重点介绍了 3,4-杂环融合香豆素的重要进展，为药物化学家在未来设计和制备具有显著治疗效果的生物活性杂环融合香豆素方面提供了更好的见解。
